M3258 | LMP7 inhibitor | Probechem Biochemicals

Chemical Structure : M3258

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M3258 (M 3258)

货号: PC-72402Not For Human Use, Lab Use Only.

M3258 (M 3258) is a potent, reversible, highly selective and orally acitve LMP7 inhibitor with cellular IC50 of 4.1 nM.

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生物&药学活性

M3258 (M 3258) is a potent, reversible, highly selective and orally acitve LMP7 inhibitor with cellular IC50 of 4.1 nM.
M3258 does not inhibit other constitutive proteasome and immunoproteasome subunits (IC50>2.5 uM).
M3258 demonstrated strong antitumor efficacy in multiple myeloma xenograft models.
M3258 treatment led to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells both in vitro and in vivo.
M3258 showed superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib.

物理化学性质&存储条件

分子量	329.159
分子式	C17H20BNO5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	((R)-2-(benzofuran-3-yl)-1-((1S,2R,4R)-7-oxabicyclo[2.2.1]heptane-2-carboxamido)ethyl)boronic acid

参考文献

1. Sanderson MP, et al. Mol Cancer Ther. 2021 Aug;20(8):1378-1387.

2. Klein M, et al. J Med Chem. 2021 Jul 22;64(14):10230-10245.

M3258 (M 3258)

生物&药学活性

物理化学性质&存储条件

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M3258 (M 3258)

生物&药学活性

物理化学性质&存储条件

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